Chalcogen Bonded Directly To Ring Carbon Of The Five-membered Hetero Ring Patents (Class 514/418)
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Patent number: 6103752Abstract: Compounds of formula (I) ##STR1## wherein R and R.sup.1 are hydrogen, C.sub.1-4 alkyl or are linked to form a ring,A is a cycloalkyl or alkyl-cycloalkyl group,n is an integer from 0 to 3,W is an optionally substituted 5- or 6-membered heterocyclic ring; or W is an optionally substituted aryl, heteroaryl, aryloxy or thiophenoxy group; orW is a group --SO.sub.2 NR.sup.6 R.sup.7 --NHC(O)R.sup.6 R.sup.7 or --C(O)NHR.sup.6 R.sup.7 ;are useful in treating clinical conditions for which a "5-HT.sub.1 -like" receptor agonist is indicated.Type: GrantFiled: February 23, 1999Date of Patent: August 15, 2000Assignee: Glaxo Wellcome Inc.Inventors: Robert Charles Glen, David Lawrence Selwood, Graeme Richard Martin, Christopher James Foster
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Patent number: 6090839Abstract: The instant invention is concerned with aryl and heteroaryl oxyacetic acid type compounds which are useful antidiabetic compounds. Compositions and methods for the use of the compounds in the treatment of diabetes and related diseases and for lowering triglyceride levels are also disclosed.Type: GrantFiled: December 19, 1997Date of Patent: July 18, 2000Assignee: Merck & Co., Inc.Inventors: Alan D. Adams, Derek Von Langen, Richard L. Tolman, Hiroo Koyama
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Indolin-2-one derivatives, method for preparing them and pharmaceutical compositions containing them
Patent number: 6090818Abstract: The invention relates to compounds with formula (I), a process for their preparation and pharmaceutical compositions containing them.Type: GrantFiled: June 14, 1999Date of Patent: July 18, 2000Assignee: Sanofi-SynthelaboInventors: Loic Foulon, Claudine Serradeil-Le Gal, Gerard Valette -
Patent number: 6083515Abstract: Nonsteroidal antiinflammatory drugs which have been substituted with a nitrogen monoxide group; compositions comprising (i) a nonsteroidal antiinflammatory drug, which can optionally be substituted with a nitrogen monoxide group and (ii) a compound that directly donates, transfers or releases a nitrogen monoxide group (preferably as a charged species, particularly nitrosonium); and methods of treatment of inflammation, pain, gastrointestinal lesions and/or fever using the compositions are disclosed. The compounds and compositions protect against the gastrointestinal, renal and other toxicities that are otherwise induced by nonsteroidal antiinflammatory drugs.Type: GrantFiled: January 22, 1999Date of Patent: July 4, 2000Assignee: NitroMed, Inc.Inventors: David S. Garvey, L. Gordon Letts, H. Burt Renfroe, Sang William Tam
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Patent number: 6075044Abstract: The use of certain heterocyclic derivatives for treating parasitic protozoa infections in mammals, in particular bovine trichomoniasis and giardiasis, is disclosed.Type: GrantFiled: July 17, 1998Date of Patent: June 13, 2000Assignee: The Regents of the University of CaliforniaInventors: Ching C. Wang, John Somoza, Jon P. Page, Ronaldus Marcellus Alphonsus Knegtel, Irwin D. Kuntz, Connie M. Oshiro, A. Geoffrey Skillman
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Patent number: 6071949Abstract: The present method provides a method for treating an epithelial cell-derived cancer in a subject in need of such treatment which comprises administering to the subject an amount of a 5-lipoxygenase inhibitor or derivative thereof effective to treat the epithelial cell-derived cancer. The present invention also provides a method for preventing an epithelial cell-derived cancer in a subject in need of such prevention which comprises administering to the subject an amount of a 5-lipoxygenase inhibitor effective to prevent the epithelial cell-derived cancer. Suitable 5-lipoxygenase inhibitors useful for the methods of the present invention preferably include 2-(12-Hydroxydodeca-5,10-dinyl)-3,5,6-trimethyl-1,4-benzoquinone and derivatives thereof; Nordihydroguaiaretic acid and derivatives; and 3-[1-(4-chlorobenzyl)-3-t-butyl-thio-t-isopropyl-indol-2-yl]-2-2-dimethylp ropanoic acid and derivatives thereof.Type: GrantFiled: December 3, 1996Date of Patent: June 6, 2000Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: James L. Mulshine, Marti Jett
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Patent number: 6069164Abstract: A method for treating circadian rhythm phase disorders is described. The invention provides methods to specifically advance or delay the phase of certain circadian rhythms in humans. The disclosed methods relate to the administration of melatonin at times determined with relation to the time of dim light endogenous melatonin onset. Embodiments capable of alleviating the effects of jet lag, winter depression and shiftwork sleep disturbance are provided.Type: GrantFiled: January 6, 1997Date of Patent: May 30, 2000Assignee: Oregon Health Sciences UniversityInventors: Alfred J. Lewy, Robert L. Sack
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Patent number: 6066663Abstract: The invention relates to derivatives of general formula I ##STR1## The invention also relates to pharmaceutical and cosmetic compositions comprising derivatives of general formula I.Type: GrantFiled: August 11, 1998Date of Patent: May 23, 2000Assignees: CEMAF, Laboratories Besins-Iscovesco S.A.Inventors: Jean-Bernard Fourtillan, Marianne Fourtillan, Jean-Claude Jacquesy, Marie-Paule Jouannetaud, Bruno Violeau, Omar Karam
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Patent number: 6063806Abstract: A heterocyclic derivative of the formula (I) ##STR1## wherein each symbol is as defined in the specification, and pharmaceutically acceptable salts thereof. The compound (I) of the present invention and pharmaceutically acceptable salts thereof exhibit superior ACAT inhibitory activity and lipoperoxidation inhibitory activity in mammals, and are useful as ACAT inhibitors and lipoperoxidation inhibitors. Specifically, they are useful for the prophylaxis and treatment of arteriosclerosis, hyperlipemia, arteriosclerosis in diabetes, and cerebrovascular and cardiovascular ischemic diseases.Type: GrantFiled: April 3, 1998Date of Patent: May 16, 2000Assignee: Kyoto Pharmaceutical Industries, Ltd.Inventors: Shoji Kamiya, Hiroaki Shirahase, Hiroshi Matsui, Shohei Nakamura, Katsuo Wada
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Patent number: 6060500Abstract: This invention relates to a method for inhibiting bome resorption in a patient with periodotal disease by administering 3-[1-(4-chlorolbenzyl)-3-t-butyl-thio-t-isopropylindol-2-yl]-2,2dimethylpr opanoic acid.Type: GrantFiled: December 27, 1996Date of Patent: May 9, 2000Assignee: Board of Regents, The University of Texas SystemInventors: Lynda F. Bonewald, G.R. Mundy, Wolf E. Gallwitz
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Patent number: 6051593Abstract: The present invention relates to novel 3-(cycloalkanoheteroarylidenyl)-2-indolinone compounds and physiologically acceptable salts and prodrugs thereof which are expected to modulate the activity of protein tyrosine kinases and therefore to be useful in the prevention and treatment of protein tyrosine kinase related cellular disorders such as cancer.Type: GrantFiled: June 19, 1998Date of Patent: April 18, 2000Assignee: Sugen, Inc.Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
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Patent number: 6028085Abstract: Prodrugs of 5HT.sub.Type: GrantFiled: September 30, 1998Date of Patent: February 22, 2000Assignee: SmithKline Beecham plcInventor: Steven Mark Bromidge
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Patent number: 6025369Abstract: The present invention relates to the novel finding that homocysteine affects the initiation and/or progress of atherosclerosis via a receptor-mediated growth factor effect on vascular smooth muscle cells. This growth factor effect can be inhibited by N-methyl-D-aspartate antagonists via a unique receptor that is in the NMDA receptor family. Through the use of cloning and other procedures, this homocysteine receptor can be characterized in order to develop novel pharmacologic strategies that the address the receptor for the prevention and treatment of atherosclerosis.Type: GrantFiled: May 2, 1997Date of Patent: February 15, 2000Assignee: The Board of Regents of the University NebraskaInventors: Thomas H. Rosenquist, Daniel T. Monaghan, Preston F. Gadson, Vincent J. Andaloro
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Patent number: 6011045Abstract: The present invention relates to compounds of the formula IA--B--D--E--F--G (I)in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as medicaments. The compounds of the invention are used as vitronectin receptor antagonists and as inhibitors of bone resorption.Type: GrantFiled: December 22, 1997Date of Patent: January 4, 2000Assignees: Hoechst Aktiengesellschaft, Genentech, Inc.Inventors: Volkmar Wehner, Hans Ulrich Stilz, Anuschirwan Peyman, Jochen Knolle, Jean-Marie Ruxer, Denis Carniato, Jean-Michel Lefrancois, Thomas Richard Gadek, Robert McDowell
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Patent number: 6001866Abstract: This invention provides a method for treating or preventing inflammation or atherosclerosis in mammals comprising administering an effective amount of a 15-LO inhibitor of Formula I: ##STR1## wherein: R.sup.1 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sup.2, R.sup.3, R.sup.4, and R.sup.5 independently are hydrogen, C.sub.1 -C.sub.6 alkyl, nitro, halo, CN, OR.sup.6, NR.sup.6 R.sup.7, --CO.sub.2 R.sup.6, CONR.sup.6 R.sup.7, CH.sub.2 OR.sup.6, or CH.sub.2 NR.sup.6 R.sup.7, and R.sup.2 and R.sup.3, and R.sup.4 and R.sup.5, when attached to adjacent ring atoms, can be --(CH.sub.2).sub.3 or 4 --;in which R.sup.6 and R.sup.7 independently are hydrogen, C.sub.1 -C.sub.6 alkyl, phenyl or benzyl, and when taken together with the nitrogen to which they are attached, R.sup.6 and R.sup.7 can complete a cyclic ring having from 3 to 7 carbon atoms; ##STR2## in which R.sup.8, R.sup.8', R.sup.9, and R.sup.9' independently are hydrogen or C.sub.1 -C.sub.6 alkyl, n is 0, 1, or 2, and Z.sup..crclbar.Type: GrantFiled: March 20, 1998Date of Patent: December 14, 1999Assignee: Warner-Lambert CompanyInventors: Joseph A. Cornicelli, Bradley D. Tait, Bharat K. Trivedi
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Patent number: 5998463Abstract: This invention relates to certain 5-acyl-2-oxo-indole-3-carboxamides useful as inhibitors of glycogen phosphorylase, methods of treating glycogen phosphorylase dependent diseases or conditions with such compounds and pharmaceutical compositions comprising such compounds. This invention also relates to pharmaceutical compositions comprising those 5-acyl-2-oxo-indole-3-carboxamides in combination with antidiabetes agents and methods of treating glycogen phosphorylase dependent diseases or conditions with such compositions.Type: GrantFiled: February 16, 1999Date of Patent: December 7, 1999Assignee: Pfizer IncInventors: Bernard Hulin, Reinhard Sarges
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Patent number: 5994388Abstract: The present invention relates to inhibition of angiogenesis and the treatment of diseases mediated by angiogenesis. Particularly, the invention relates to the inhibition of neovascularization and the treatment of cancer. The invention further relates to the use of cytochalasin derivatives for the inhibition of angiogenesis and the treatment of angiogenesis associated diseases. The invention also relates to new isoindolinone compounds, compositions containing them, and methods of inhibiting angiogenesis and treating angiogenesis associated diseases with the isoindolinone derivatives.Type: GrantFiled: March 17, 1998Date of Patent: November 30, 1999Assignee: The Children's Medical Center CorporationInventors: Taturo Udagawa, Robert J. D'Amato, Jamshed H. Shah
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Patent number: 5990145Abstract: The present invention relates to compounds of the formula I,A--B--D--E--F--G (I)in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as medicaments. The compounds of the invention are used as vitronectin receptor antagonists and as inhibitors of bone resorption.Type: GrantFiled: December 22, 1997Date of Patent: November 23, 1999Assignees: Hoechst Aktiengesellschaft, Genentech, Inc.Inventors: Volkmar Wehner, Hans Ulrich Stilz, Anuschirwan Peyman, Karlheinz Scheunemann, Jean-Marie Ruxer, Denis Carniato, Jean-Michel Lefrancois, Thomas Richard Gadek, Robert McDowell
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Patent number: 5985926Abstract: There is disclosed a method of preventing or delaying the occurrence of acquired immunodeficiency syndrome (AIDS) in human immunodeficiency virus (HIV) seropositive humans by administering an effective amount of a compound that inhibits cellular signaling through a specific phospholipid-based cellular signaling and signal amplification pathway. The invention further provides a method for preventing or delaying clinical symptoms of a group of viral diseases wherein the viral disease is mediated by host cell viral replication. The invention provides an advantage by attacking host cellular signaling mechanisms to prevent the development of drug resistance from rapidly mutating viruses.Type: GrantFiled: February 10, 1997Date of Patent: November 16, 1999Assignee: Cell Therapeutics, Inc.Inventors: David W. Leung, Gail E. Underiner, Jack W. Singer
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Patent number: 5977130Abstract: The present invention is directed to an intimal hypertrophy inhibitor containing as the active ingredient an oxyindole derivative represented by the following formula (I) or a salt thereof: ##STR1## (wherein R.sup.1 represents a hydrogen atom; a phenyl group which may be substituted by a lower alkyl group, a lower alkoxy group, a lower alkylaminoalkoxy group, a hydroxy group, an amino group, a lower alkylamino group, or a halogen atom; or a pyridyl group which may be substituted by a lower alkyl group, a lower alkoxy group, a lower alkylaminoalkoxy group, a hydroxy group, an amino group, a lower alkylamino group, a halogen atom, a lower alkoxycarbonyl group, or a carboxyl group; R.sup.2 represents a phenyl group which may be substituted; or a pyridyl group which may be substituted by a lower alkyl group, a lower alkoxy group, a lower alkylaminoalkoxy group, a hydroxy group, an amino group, a lower alkylamino group, a halogen atom, a lower alkoxycarbonyl group, or a carboxyl group; R.sup.Type: GrantFiled: September 10, 1997Date of Patent: November 2, 1999Assignee: Taiho Pharmeutical Co., Ltd.Inventors: Atsushi Sato, Tetsuji Asao, Yuichi Hagiwara, Makoto Kitade, Yasundo Yamazaki
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Patent number: 5972988Abstract: A method is disclosed for the treatment of chronic bronchitis by administering to a mammal in need thereof a therapeutically effective amount of a 1H-indole-3-glyoxylamide compound.Type: GrantFiled: March 12, 1998Date of Patent: October 26, 1999Assignee: Eli Lilly and CompanyInventor: William Louis Macias
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Patent number: 5948808Abstract: Provided in the present invention are compounds and compositions of substituted indole-3-carbinols and diindolylmethane suitable for treating estrogen-dependent tumors. Also provided are methods of treating such cancerous-conditions.Type: GrantFiled: March 7, 1997Date of Patent: September 7, 1999Assignee: The Texas A&M University SystemInventor: Stephen H. Safe
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Patent number: 5945413Abstract: This invention relates to a novel class of compounds that are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting aspartyl protease activity and methods for treating viral infections using the compounds and compositions of this invention.Type: GrantFiled: September 30, 1996Date of Patent: August 31, 1999Assignee: Vertex Pharmaceuticals IncorporatedInventors: Roger Dennis Tung, Francesco Gerald Salituro, David D. Deininger, Govinda Rao Bhisetti, Christopher Todd Baker, Andrew Spaltenstein
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Patent number: 5939452Abstract: The invention relates to novel benzopyran and other benzo-fused leukotriene B.sub.4 (LTB.sub.4) antagonists of formula I and the pharmaceutically acceptable salts thereof, to pharmaceutical compositions containing such compounds, and to a method of using such compounds as LBT.sub.4 antagonists. The compounds of the invention inhibit the action of LTB.sub.4 and are therefore useful in the treatment of LTB.sub.4 induced illnesses such as inflammatory disorders including rheumatoid arthritis, osteoarthritis, inflammatory bowel disease, psoriasis and other skin disorders such as eczema, erythema, pruitus and acne, stroke and other forms of reperfusion injury, graft rejection, autoimmune diseases, asthma and other conditions where marked neutrophil infiltration occurs.Type: GrantFiled: April 9, 1997Date of Patent: August 17, 1999Assignee: Pfizer IncInventors: Mark Anthony Dombroski, Kevin Koch, Anthony Daniel Piscopio
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Patent number: 5919809Abstract: This invention relates to novel 3-substituted-2-oxindole derivatives of the formula ##STR1## and the pharmaceutically-acceptable salts thereof which are inhibitors of prostaglandin H.sub.2 synthase, 5-lipoxygenase and interleukin-1 biosynthesis. The compounds of the invention are useful as inhibitors of prostaglandin H.sub.2 synthase and interleukin-1 biosynthesis, per se, and as analgesic, antiinflammatory and antiarthritic agents in the treatment of chronic inflammatory diseases. This invention also relates to pharmaceutical compositions comprising said 3-substituted-2-oxindole derivatives; to methods of inhibiting prostaglandin H.sub.2 synthase and biosynthesis of interleukin-1; and to treating chronic inflammatory diseases in a mammal with said compounds. Further, this invention relates to certain novel carboxylic acids useful as intermediates in the preparation of the 3-substituted-2-oxindole derivatives of this invention and to a process for the preparation of the 3-substituted-2-oxindole derivatives.Type: GrantFiled: November 4, 1993Date of Patent: July 6, 1999Assignee: Pfizer Inc.Inventors: Frederick J. Ehrgott, Carl J. Goddard, Gary R. Schulte
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Patent number: 5919792Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as vitronectin receptor antagonists. The vitronectin receptor antagonist compounds of the present invention are .alpha.v.beta.3 antagonists, .alpha.v.beta.5 antagonists or dual .alpha.v.beta.3/.alpha.v.beta.5 antagonists useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation and tumor growth.Type: GrantFiled: October 28, 1997Date of Patent: July 6, 1999Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, George D. Hartman, William F. Hoffman, Nathan C. Ihle
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Patent number: 5919790Abstract: The present invention relates to compounds that are inhibitors of interleukin-1.beta. converting enzyme that have the Formula II ##STR1## This invention also relates to a method of treatment of stroke, inflammatory diseases, septic shock, reperfusion injury, Alzheimer's disease, shigellosis, and to a pharmaceutically acceptable composition that contains a compound that is an inhibitor of interleukin-1.beta. converting enzyme.Type: GrantFiled: October 2, 1997Date of Patent: July 6, 1999Assignees: Warner-Lambert Company, BASF AktiengesellsschaftInventors: Hamish John Allen, Kenneth Dale Brady, Bradley William Caprathe, Paul Galatsis, John Lodge Gilmore, Sheryl Jeanne Hays, Robert Vincent Talanian, Nigel Walker, Joseph Scott Warmus
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Patent number: 5891902Abstract: The present invention relates to indole derivatives represented by formula (I): ##STR1## wherein R.sup.1 and R.sup.2 independently represent hydrogen, lower alkyl, hydroxy, lower alkoxy, halogen, --O--(CH.sub.2).sub.n --OR.sup.5, or ##STR2## R.sup.3 represents hydrogen, lower alkyl, or ##STR3## R.sup.4 represents hydroxy, lower alkoxy, substituted or unsubstituted aryloxy, or --NR.sup.10 R.sup.11, and X represents CO or SO.sub.2, with the proviso that when R.sup.3 is hydrogen or lower alkyl, and X is CO, R.sup.4 is --NR.sup.10 R.sup.11, or pharmaceutically acceptable salts thereof.Type: GrantFiled: July 15, 1996Date of Patent: April 6, 1999Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Daisuke Machii, Haruki Takai, Nobuo Kosaka, Hisakatsu Seo, Tomomi Sugiyama, Joji Nakamura, Hiroyuki Ishida, Katsushige Gomi, Soichiro Sato, Masako Uchii, Koji Suzuki
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Patent number: 5886020Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.Type: GrantFiled: June 5, 1996Date of Patent: March 23, 1999Assignee: Sugen, Inc.Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
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Patent number: 5883116Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.Type: GrantFiled: June 5, 1996Date of Patent: March 16, 1999Assignee: Sugen, Inc.Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
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Patent number: 5883113Abstract: The present invention relates to organic molecules apable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal ell proliferation.Type: GrantFiled: June 5, 1996Date of Patent: March 16, 1999Assignee: Sugen, Inc.Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
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Patent number: 5880141Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.Type: GrantFiled: June 7, 1995Date of Patent: March 9, 1999Assignee: Sugen, Inc.Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
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Patent number: 5861426Abstract: New compounds and their compositions having anti-inflammatory, analgesic and anti-thrombotic activities, of the general formula: A--X.sub.1 --NO.sub.2 or their salts, wherein: A is R(COX.sub.u).sub.t, wherein t is zero or 1 and u is zero or 1; and X is O, NH or NR.sub.1C wherein R.sub.1C is C.sub.1 -C.sub.10 alkyl; and R is(Ia) wherein R.sub.1 is acetoxoy, preferably n ortho-position with respect to --CO-- and R.sub.2 is hydrogen; or derivatives of acetylsalylsalicyclic acid; and X.sub.1 is --YO-- wherein Y is C.sub.1 -C.sub.20 alkylene, C.sub.5 -C.sub.7 cycloalkylene, oxy-alkyl derivatives and oxy-methyl benzyl derivatives.Type: GrantFiled: March 6, 1997Date of Patent: January 19, 1999Assignee: Nicox S.A.Inventors: Piero Del Soldato, Francesco Sannicolo
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Patent number: 5859017Abstract: In a method for treating or preventing allergy or allergic disorders an effective amount of a compound that inhibits intracellular generation of phosphatidic acid and diacylglycerol is administered. The intracellular generation of phosphatidic acid and diacylglycerol results from allergen presentation or mast cell/basophil activation.Type: GrantFiled: April 1, 1994Date of Patent: January 12, 1999Assignee: Cell Therapeutics, Inc.Inventors: Elisa Eiseman, Emer Clarke, Jack W. Singer, Stuart L. Bursten
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Patent number: 5849764Abstract: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.Type: GrantFiled: December 5, 1996Date of Patent: December 15, 1998Assignee: Merck & Co., Inc.Inventors: Mark Goulet, Lin Chu, Thomas F. Walsh, Michael H. Fisher, Narindar N. Girotra, Matthew J. Wyvratt, Peter Lin, Wallace T. Ashton
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Patent number: 5849710Abstract: The present invention relates to indol-3-ylmethylene-2-oxindole derivatives which are useful as tyrosine kinase inhibitors. The compounds are suitable for use as anti-proliferative agents, anti-metastatic agents, anti-cancer agents, and in the control of angiogenesis and in inhibiting the development of atheromatous and an immunomogulating agents.Type: GrantFiled: December 4, 1996Date of Patent: December 15, 1998Assignee: Pharmacia & Upjohn S.p.A.Inventors: Carlo Battistini, Dario Ballinari, Antonella Ermoli, Sergio Penco, Sergio Vioglio
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Patent number: 5849756Abstract: Pharmaceutical compositions for the modulation of the immune reaction of warm blooded animals that are derivatives of the 2-oxindole-3-acetic acid or the 2-oxo-1,2,3,4-tetrahydroquinoline-4-carboxylic acid are described, and whereby the derivatives can optionally be in an equilibrium with each other.The derivatives included in the pharmaceutical compositions comprise those compounds which are already described in the literature and also new compounds.Furthermore, new derivatives of the the 2-oxindole-3-acetic acid and the 2-oxo-1,2,3,4-tetrahydroquinoline-4-carboxylic acid are described, particularly also the the pure antipodes of the mixture of enantiomeres of the 2-oxo-1,2,3,4-tetrahydroquinoline-4-carboxylic acid.Type: GrantFiled: May 26, 1995Date of Patent: December 15, 1998Assignee: Cerbios-Pharma SAInventors: Ulrich Burger, Jean-Claude Jaton, Fabrizio Marazza, Ari Lewenstein, Francis M. Sirotnak
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Patent number: 5849782Abstract: Methods for inhibiting a nitric oxide-mediated pathological condition and a neurodegenerative disease such as Parkinson's disease, Huntington's disease, Alzheimers's disease, and amyotrophic lateral sclerosis in a human patient, comprising administering an effective amount of a nitroindazole capable of inhibiting a neuronal nitric oxide synthase.Type: GrantFiled: July 12, 1996Date of Patent: December 15, 1998Assignee: The General Hospital CorporationInventor: M. Flint Beal
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Patent number: 5847155Abstract: A series of aromatic pyrrolidine derivatives and suitable pharmaceutically acceptable salts thereof are disclosed. These compounds are useful as PEP inhibitors in the treatment of Alzheimer's disease, amnesia, dementia, anxiety ischemia, or stroke.Type: GrantFiled: January 26, 1996Date of Patent: December 8, 1998Assignee: Pfizer IncInventors: W. Stephen Faraci, Arthur A. Nagel, Robin W. Spencer, Fredric J. Vinick
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Patent number: 5840745Abstract: Novel hydrosoluble 3-arylidene-2-oxindole derivatives, having tyrosine kinase inhibitor activity, encompassed by general formula (I), wherein m is zero, 1 or 2; A is a bicyclic ring chosen from tetralin, naphthalene, quinoline and indole; R.sup.1 is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.2 -C.sub.6 alkanoyl; one of R.sup.2 and R.sup.3 independently is hydrogen and the other is a substituent selected from: a C.sub.1 -C.sub.6 alkyl group substituted by 1, 2 or 3 hydroxy groups; --SO.sub.3 R.sup.4 in which R.sup.4 is hydrogen or C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by 1, 2 or 3 hydroxy groups; --SO.sub.2 NHR.sup.5 in which R.sup.5 is as R.sup.4 defined above or a --(CH.sub.2).sub.n --N(C.sub.1 -C.sub.6 alkyl).sub.2 group in which n is 2 or 3; --COOR.sup.6 in which R.sup.6 is C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by phenyl or by 1, 2 or 3 hydroxy groups or phenyl; --CONHR.sup.7 in which R.sup.7 is hydrogen, phenyl or C.sub.1 -C.sub.Type: GrantFiled: September 25, 1996Date of Patent: November 24, 1998Assignee: Pharmacia S. p. A.Inventors: Franco Buzzetti, Maria Gabriella Brasca, Antonio Longo, Dario Ballinari
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Patent number: 5834504Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.Type: GrantFiled: June 5, 1996Date of Patent: November 10, 1998Assignee: Sugen, Inc.Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
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Patent number: 5824677Abstract: Disclosed are compounds having a straight or branched aliphatic hydrocarbon structure of formula I: ##STR1## In formula I, n is an integer from one to four and m is an integer from four to twenty. Independently, R.sub.1 and R.sub.2 are hydrogen, a straight or branched chain alkyl, alkenyl or alkynyl of up to twenty carbon atoms in length or --(CH.sub.2).sub.w R.sub.5. If R.sub.1 or R.sub.2 is --(CH.sub.2).sub.w R.sub.5, w may be an integer from one to twenty and R.sub.5 may be an hydroxyl, halo, C.sub.1-8 alkoxyl group or a substituted or unsubstituted carbocycle or heterocycle. Alternatively, R.sub.1 and R.sub.2 may jointly form a substituted or unsubstituted, saturated or unsaturated heterocycle having from four to eight carbon atoms, N being a hetero atom of the resulting heterocyle. R.sub.3 may be either hydrogen or C.sub.13. In the compounds, a total sum of carbon atoms comprising R.sub.1 or R.sub.2, (CH.sub.2).sub.n and (CH.sub.2).sub.m does not exceed forty. R.sub.Type: GrantFiled: June 7, 1995Date of Patent: October 20, 1998Assignee: Cell Therapeutics, Inc.Inventors: J. Peter Klein, Gail E. Underiner, Anil M. Kumar
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Patent number: 5821256Abstract: Novel compounds of the formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and X have the meaning indicated in claim 1, and their salts exhibit endothelin receptor-antagonistic properties.Type: GrantFiled: August 15, 1996Date of Patent: October 13, 1998Assignee: Merck Patent Gesellschaft mit Beschrankter HaftungInventors: Dieter Dorsch, Mathias Osswald, Werner Mederski, Claudia Wilm, Claus J. Schmitges, Maria Christadler
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Patent number: 5817690Abstract: A compound of the formula I: ##STR1## in which Y is hydrogen, halogen or lower alkoxy; R.sub.1 is hydrogen, lower alkyl or aryl(lower)alkyl; R.sub.2 is hydrogen, lower alkyl or --(CH.sub.2).sub.n X.sub.p Ar, where X is oxygen or carbonyl; Ar is cycloalkyl, aryl or arylaryl, oxindolyl, benzimidazolyl, indolyl, 2-oxobenzimidazolyl or 2-thioxobenzimidazolyl; or R.sub.1 and R.sub.2, taken together with the nitrogen atom to which they are attached, complete a 3,4-dihydro-1H-isoquinolinyl or 1,3-dihydro-isoindolyl; n is one of the integers 1,2,3,4,5 or 6; p is one of the integers 0 or 1; or a pharmaceutically acceptable salt thereof are inhibitors of dopamine synthesis and release, useful in the treatment of schizophrenia, Parkinson's Disease, Tourette's Syndrome, alcohol addiction, cocaine addiction, and addiction to analogous drugs.Type: GrantFiled: August 12, 1997Date of Patent: October 6, 1998Assignee: American Home Products CorporationInventor: Richard Eric Mewshaw
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Patent number: 5807883Abstract: Disclosed is a 2-oxoindoline derivative represented by the formula (I): ##STR1## wherein Ring A represents a benzene ring which is substituted in the 5-position or 6-position by a lower alkyl group or lower alkoxy group, R.sup.1 represents a phenyl group which is substituted by a halogen atom, a lower alkyl group or a lower alkoxy group, R.sup.2 represents a naphthyl group, indolyl group, isoquinolyl group, benzimidazolyl group or a group represented by the formula: ##STR2## wherein n represents 1 or 2, R.sup.3 represents a lower alkyl group which is substituted by a carboxyl group, a cyano group or a tetrazolyl group, O represents a single bonding arm, and Y represents a single bonding arm,or a pharmaceutically acceptable salt thereof.Type: GrantFiled: May 24, 1996Date of Patent: September 15, 1998Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Koichiro Yamada, Masataka Hikota, Toshiro Shikano, Masaaki Nagasaki
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Patent number: 5801181Abstract: Therapeutic compounds have the formula:(X)j--(core moiety),J being an integer from one to three, the core moiety having at least one, five- to seven-membered ring and X being a racemic mixture, R or S enantiomer, slovate, hydrate, or salt of: ##STR1## *C is a chiral carbon atom, n is an integer from one to four (preferably from one to three), one or more carbon atoms of (CH.sub.2).sub.n may be substituted by a keto or hydroxy group, and m is an integer from one to fourteen. Independently, R.sub.1 and R.sub.2 may be a hydrogen, a straight or branched chain alkane or alkene of up to twelve carbon atoms in length, or --(CH.sub.2).sub.w R.sub.5, w being an integer from two to fourteen and R.sub.5 being a mono-, di- or tri-substituted or unsubstituted aryl group, substituents on R.sub.5 being hydroxy, chloro, fluoro, bromo, or C.sub.1-6 alkoxy. Or jointly, R.sub.1 and R.sub.Type: GrantFiled: June 7, 1995Date of Patent: September 1, 1998Assignee: Cell Therapeutics, Inc.Inventors: John Michnick, Gail E. Underiner, J. Peter Klein, Glenn C. Rice
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Patent number: 5795902Abstract: The present invention relates to a pharmaceutical preparation comprising: (A) at least one triglyceride or propylene glycol diester of fractionated coconut oil fatty acids; and (B) at least one carboxamide compound of the formula I. The composition renders the carboxamides of formula I more storage-stable and less susceptible to hydrolysis. Methods of using the composition to inhibit activation of collagenase, treating inflammatory disease, and eliciting an analgesic response are also disclosed.Type: GrantFiled: September 19, 1996Date of Patent: August 18, 1998Assignee: Pfizer Inc.Inventor: Imram Ahmed
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Patent number: 5789404Abstract: 3-Substituted 1-arylindole compounds are provided having general formula (I) ##STR1## wherein Ar is an optionally substituted aryl group; X represents a divalent hydrocarbon group, methyleneoxy or -thioxo; R.sup.1 -R.sup.4 are hydrogen or other substituents; R.sup.5 is hydrogen, alkyl, alkenyl, etc.; R.sup.6 and R.sup.7 are independently hydrogen, alkyl, alkenyl, etc.; R.sup.8 is alkyl, alkenyl or R.sup.8 represents a group of formula 1a or 1b; wherein n is an integer from 2-8; W is O or S; U is N or CH; Z is (CH.sub.2).sub.m, m being 2 or 3, 1,2-phenylene optionally substituted with halogen or trifluoromethyl, CH.dbd.CH, COCH.sub.2 or CSCH.sub.2 ; V is O, S, CH.sub.2 or NR.sup.10, wherein R.sup.10 is hydrogen, alkyl, alkenyl, cycloalkyl, etc.; U.sup.1 is O, S, CH.sub.2 or a group NR.sup.11, wherein R.sup.11 is hydrogen, alkyl, alkenyl, etc.; and V.sup.1 is NR.sup.12 R.sup.13, OR.sup.14, SR.sup.15 or CR.sup.16 R.sup.17 R.sup.18, where R.sup.12 -R.sup.18 are as the R.sup.10 substituents; R.sup.Type: GrantFiled: August 12, 1996Date of Patent: August 4, 1998Assignee: H. Lundbeck A/SInventors: Kim Andersen, Jens Kristian Perregaard
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Patent number: 5783543Abstract: A carpet cleaning composition comprising: (a) a powder-form solid adsorbent; (b) rollable particles of porous material, each particle having a length greater than 1 mm, and a diameter equal to at least 10% of the length of the particle; and (c) water.Type: GrantFiled: October 30, 1996Date of Patent: July 21, 1998Assignee: Henkel Kommanditgesellschaft auf AktienInventors: Theo Fleckenstein, Alexander Ditze, Franz Kresse, Thomas Hahn
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Patent number: 5783605Abstract: Cancer cells are blocked from entering differentiation pathways because of abnormal methylation enzymes, which are responsible for keeping cancer cells in cycling state. Effective differentiation inducers are those capable of acting directly or indirectly to convert abnormal methylation enzymes into normal enzymes, thereby enabling cancer cells to undergo terminal differentiation. Differentiation employing inducer alone often can not reach completion because of the damage created by the inducer. Such damage can be prevented if differentiation is induced in the presence of helper inducers, which are basically inhibitors of the component enzymes of methylation. Thus, differentiation induced in the presence of helper inducers is more likely to reach completion. Therefore, helper inducers are essential components of differentiation therapy, not just merely to potentiate the activity of differentiation inducers.Type: GrantFiled: October 15, 1996Date of Patent: July 21, 1998Inventors: Sheng-Chu Kuo, Jau-Hong Lee